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Cyclo(his-pro) TFA

产品编号 T61171 CAS 936749-56-3

Cyclo(his-pro) TFA, an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone, has shown inhibitory effects on NF-κB nuclear accumulation. Additionally, it possesses the ability to cross the blood-brain barrier and impact various inflammatory and stress responses [1, 2].

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Cyclo(his-pro) TFA, CAS 936749-56-3

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其他形式的 Cyclo(his-pro) TFA:

Cyclo(his-pro)
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生物活性

化学信息

存储 & 溶解度

产品描述	Cyclo(his-pro) TFA, an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone, has shown inhibitory effects on NF-κB nuclear accumulation. Additionally, it possesses the ability to cross the blood-brain barrier and impact various inflammatory and stress responses [1, 2].
体外活性	Cyclo(his-pro) TFA (Cyclo(histidyl-proline) TFA; 50 μM; 1-48 hours) increases the nuclear level of Nrf2 and inhibits NF-κB nuclear translocation. Cyclo(His-Pro) alone has no effect on nuclear translocation of these transcription factors [2]. Cyclo(his-pro) TFA (50 μM; prior to PQ exposure for 48 hours) abolishes protein nitration that followed paraquat (PQ) exposure and lessenes its functional consequences, as shown by decrease in cell apoptosis, detected by caspase 3 activity and by cytochrome c release [2]. Cyclo(his-pro) TFA inhibits NF-κB nuclear accumulation induced by paraquat in rat pheochromocytoma PC12 cells via the Nrf2/heme oxygenase-1 pathway [2]. Western Blot Analysis [1] Cell Line: PC12 cells Concentration: 50 μM Incubation Time: 1, 2, 4, 8, 24, 48 hours Result: Increased the nuclear level of Nrf2 and inhibited NF-κB nuclear translocation.
体内活性	Cyclo(his-pro) TFA (Cyclo(histidyl-proline) TFA; 1.8 mg/ear; topical application on the right ear; 30 min prior to TPA) reduces TPA-induced ear oedema confirming that it can exert anti-inflammatory effect [2]. Cyclo(his-pro) TFA exerts in vivo anti-inflammatory effects in the central nervous system by down-regulating hepatic and cerebral TNFα expression thereby counteracting LPS-induced gliosis. Moreover, by up-regulating Bip, Cyclo(his-pro) increases the ER stress sensitivity andtriggers the unfolded protein response to alleviate the ER stress [3]. Animal Model: Sixty two/three month-old male C57BL/6 mice (25-30 g) [2] Dosage: 1.8 mg/ear Administration: Topical application on the right ear; 30 min prior to TPA Result: Reduced TPA-induced ear oedema.

分子量	348.282
分子式	C13H15F3N4O4
CAS No.	936749-56-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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